CAS: 167465-36-3; (R)-1-(4-((1Ar,6R,10Bs)-1,1-Difluoro-1,1A,6,10B-Tetrahydrodibenzo[a,E]Cyclopropa[c][7]Annulen-6-yl)Piperazin-1-yl)-3-(Quinolin-5-Yloxy)Propan-2-Ol Trihydrochloride

该化合物是主要研究其在癌症治疗中的潜在作用的化学化合物,特别是在克服白血病和其他恶性肿瘤中的药物抗药性方面的潜在作用,是P-glycoprotein(P-gp)增殖泵的选择性抑制剂,该泵在癌症细胞中经常表现过量,通过将治疗剂从细胞中驱逐出,有助于多种药物的抗药性.该化合物的特点是其三氢氯化盐形式,它增强了其在水溶性溶性,便于其在生物研究中的使用.Zosuquidar在各种临床和临床环境中进行了评估,表明它能够使抗病性癌症细胞对化学疗法有敏感认识,其药理学特征包括药物疗法和潜在副作用在内的所有特性都在临床试验中继续探索.

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欧盟法规

C&L通报

上下游产品

5-[(2R)-oxiranylmethoxy]-quinoline

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    专利信息


    专利号:US-12391691-B2
    优先权日:2018-11-16
    标题:Synthesis of key intermediate of KRAS G12C inhibitor compound
    发明人:PARSONS ANDREW THOMAS; COCHRAN BRIAN MCNEIL; POWAZINIK IV WILLIAM; CAPORINI MARC ANTHONY
    权利人:AMGEN INC
    摘要:The present invention relates to an improved, efficient, scalable process to prepare intermediate compounds, such as compound 5M, having the structure n nuseful for the synthesis of compounds that target KRAS G12C mutations, such as

    专利号:US-2025206736-A1
    优先权日:2019-11-14
    标题 :Synthesis of kras g12c inhibitor compound
    发明人:CORBETT MICHAEL THOMAS; CAILLE SEBASTIEN
    权利人:AMGEN INC
    摘要:The present disclosure relates to an improved, efficient, scalable process to prepare intermediate compounds, such as 2-isopropyl-4-methylpyridin-3-amine, useful for the synthesis of compounds, such as Compound 9, for the treatment of KRAS G12C mutated cancers.

    专利号:US-2025241876-A1
    优先权日:2023-07-19
    标 题:Anti-tumor compounds and methods of use thereof and synthesis thereof
    发明人:QUAY STEVEN CARL
    权利人:ATOSSA THERAPEUTICS INC
    摘要:Described herein are pharmaceutical compounds and compositions and methods of making thereof. Methods of synthesis for the compounds are described herein. The compounds or compositions described herein may exhibit aromatase inhibition activity or estrogen receptor activity. The compounds and compositions described herein may be useful in the treatment of a condition in a subject.

    专利号:US-2023192682-A1
    优先权日:2019-11-14
    标题:Improved synthesis of kras g12c inhibitor compound

    专利号:US-2023192681-A1
    优先权日:2019-11-14
    标 题 :Improved synthesis of kras g12c inhibitor compound

    专利号:US-2024279225-A1
    优先权日:2021-04-08
    标 题 :Compounds and methods for theranostic targeting of parp activity
    发明人:PISANESCHI FEDERICA; MUZZIOLI RICCARDO; GAMMON SETH; PIWNICA-WORMS DAVID
    权利人:UNIV TEXAS
    摘要:The synthesis and use of radiolabeled derivatives of poly-(ADP-ribose) (PARP) inhibitors in positron emission tomography (PET) imaging methods are disclosed. A novel non-radioactive analogue of the PARP inhibitor Talazoparib (TZ) provides a branch point for the syntheses of various radiolabeled Talazoparib derivatives. Aspects of the disclosure include such radiolabeled derivatives and TZ analogues, along with methods of use for diagnosis, treatment, imaging, and theranosis of cancer.

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    主要参考文献


    1: Infed N, Smits SH, Dittrich T, Braun M, Driessen AJ, Hanekop N, Schmitt L. Analysis of the inhibition potential of zosuquidar derivatives on selected bacterial and fungal ABC transporters. Mol Membr Biol. 2013 Mar;30(2):217-27. doi: 10.3109/09687688.2012.758876. doi: 10.1007/s10549-011-1937-9. Epub 2012 Jan 8. doi: 10.1182/blood-2010-04-277269. Epub 2010 Aug 17.
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    8: Morschhauser F, Zinzani PL, Burgess M, Sloots L, Bouafia F, Dumontet C. Phase I/II trial of a P-glycoprotein inhibitor, Zosuquidar.3HCl trihydrochloride (LY335979), given orally in combination with the CHOP regimen in patients with non-Hodgkin's lymphoma. Leuk Lymphoma. 2007 Apr;48(4):708-15. Epub 2007 Mar 23. Epub 2006 Jan 24.

    合成参考文献


    参考文献:10.1186/1742-2094-11-91
    摘要:Ashraf T, Jiang W, Hoque MT, Henderson J, Wu C, Bendayan R. Role of anti-inflammatory compounds in human immunodeficiency virus-1 glycoprotein120-mediated brain inflammation. Journal of Neuroinflammation. 2014 May 16;11(1):91. doi: 10.1186/1742-2094-11-91.
    参考文献:10.1208/s12248-015-9829-2
    摘要:Svensson EM, Acharya C, Clauson B, Dooley KE, Karlsson MO. Pharmacokinetic Interactions for Drugs with a Long Half-Life—Evidence for the Need of Model-Based Analysis. The AAPS Journal. 2015 Oct 13;18(1):171–9. doi: 10.1208/s12248-015-9829-2.
    参考文献:10.2165/00003088-200645090-00002
    摘要:Motl S, Zhuang Y, Waters CM, Stewart CF. Pharmacokinetic considerations in the treatment of CNS tumours. Clin Pharmacokinet. 2006;45(9):871–903. doi: 10.2165/00003088-200645090-00002.
    参考文献:10.1007/s10637-006-9001-z
    摘要:Jin J, Sun H, Wei H, Liu G. The anti-hepatitis drug DDB chemosensitizes multidrug resistant cancer cells in vitro and in vivo by inhibiting P-gp and enhancing apoptosis. Invest New Drugs. 2007 Apr;25(2):95–105. doi: 10.1007/s10637-006-9001-z.
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